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Development and in vivo evaluation of papain-functionalized nanoparticles
Christiane Müller1, Glen Perera1, Verena König1
1Department of Pharmaceutical Technology, University of Innsbruck, Innsbruck, Austria.
Summary
Novel nanoparticles with papain enzyme can break down intestinal mucus, improving drug delivery. These papain-grafted polyacrylic acid nanoparticles show 3x greater mucus penetration for enhanced mucosal drug absorption.
Area of Science:
- Biomaterials Science
- Drug Delivery Systems
- Gastrointestinal Research
Background:
- Intestinal mucus barrier limits drug absorption.
- Novel delivery systems are needed to overcome this barrier.
- Mucolytic enzymes can degrade mucus.
Purpose of the Study:
- Develop papain-grafted polyacrylic acid nanoparticles.
- Evaluate their ability to penetrate intestinal mucus.
- Assess their potential for enhanced mucosal drug delivery.
Main Methods:
- Ionic gelation for nanoparticle preparation.
- Rheological measurements and diffusion studies for mucus penetration.
- In vivo studies in Sprague Dawley rats.
Main Results:
- Papain-grafted nanoparticles significantly reduced mucus viscosity.
- Enzyme-functionalized particles showed 3.0-fold higher diffusion through mucus.
- Particles successfully traversed mucus and localized in the duodenum and jejunum.
Conclusions:
- Papain-grafted nanoparticles effectively overcome the intestinal mucus barrier.
- This approach offers a promising strategy for improving mucosal drug delivery.
- Mucolytic enzyme-functionalized nanoparticles represent a novel advancement in drug delivery.

